103529-16-4Relevant articles and documents
Selective and efficient access to ortho, meta and para ring-substituted phenylacetylene derivatives R-[C≡C-C6H4](x)-Y (Y:H, NO2, CN, I, NH2)
Lavastre, Olivier,Cabioch, Sandrine,Dixneuf, Pierre H.,Vohlidal, Jiri
, p. 7595 - 7604 (1997)
ortho, meta and para isomers of iodo and amino ring-substituted phenylacetylene as well as rod-like arylacetylene derivatives were prepared by a simple synthetic route involving three consecutive reactions: the palladium-catalysed carbon-carbon bond forma
Rhenium-Catalyzed Intramolecular Carboalkoxylation and Carboamination of Alkynes for the Synthesis of C3-Substituted Benzofurans and Indoles
Rong, Ming-Guang,Qin, Tian-Zhu,Zi, Weiwei
, p. 5421 - 5425 (2019)
A rhenium-catalyzed carboalkoxylation and carboamination of alkyne is reported. This reaction provides an efficient route to synthesize de novo C3-substituted benzofurans and indoles under mild conditions in moderate to good yields. Mechanistic studies re
Pyreno[2,1-b]pyrrole and bis(pyreno[2,1-b]pyrrole) as selective chemosensors of fluoride ion: A mechanistic study
Lin, Chia-I.,Selvi, Srinivasan,Fang, Jim-Min,Chou, Pi-Tai,Lai, Chin-Hung,Cheng, Yi-Ming
, p. 3537 - 3542 (2007)
(Chemical Equation Presented) Pyreno[2,1-b]pyrrole and its dimeric derivative display excellent selectivity and sensitivity for detection of fluoride ion, in comparison with chloride, bromide, iodide, acetate, dihydrogen phosphate, hydrogen sulfate, perch
1,2,3-triazoles as amide bioisosteres: Discovery of a new class of potent HIV-1 Vif antagonists
Mohammed, Idrees,Kummetha, Indrasena Reddy,Singh, Gatikrushna,Sharova, Natalia,Lichinchi, Gianluigi,Dang, Jason,Stevenson, Mario,Rana, Tariq M.
, p. 7677 - 7682 (2016)
RN-18 based viral infectivity factor (Vif), Vif antagonists reduce viral infectivity by rescuing APOBEC3G (A3G) expression and enhancing A3G-dependent Vif degradation. Replacement of amide functionality in RN-18 (IC50 = 6 μM) by isosteric heterocycles resulted in the discovery of a 1,2,3-trizole, Id (IC50 = 1.2 μM). We identified several potent HIV-1 inhibitors from a Id based library including 5ax (IC50 = 0.01 μM), 5bx (0.2 μM), 2ey (0.4 μM), 5ey (0.6 μM), and 6bx (0.2 μ M).
Phenylene ethynylene pentamers for organic electroluminescence
Anderson
, p. 4706 - 4714 (2001)
An isomeric family of eighteen triisopropylsilyl-capped phenylene ethynylene pentamers (molecular formula C60H62Si2) has been prepared by using fast parallel synthesis, for organic electroluminescence. Each pentamer was grown on a polymer support of propylaminomethylated polystyrene by using a series of palladium-catalysed reactions between aryl iodides and alkynes. "Tea bag" technology was used to carry out several different reactions simultaneously in the same flask. Here I present the syntheses of the materials, compare their photoluminescence both in solution and in the solid state (amorphous thin films) and describe the incorporation of the most promising pentamer into organic electroluminescence devices.
Gold-Catalyzed Synthesis of π-Extended Carbazole-Based Systems and their Application as Organic Semiconductors
Hendrich, Christoph M.,Hannibal, Valentin D.,Eberle, Lukas,Hertwig, Leif E.,Zschieschang, Ute,Rominger, Frank,Rudolph, Matthias,Klauk, Hagen,K. Hashmi, A. Stephen
, p. 1401 - 1407 (2021)
Herein we describe a gold-catalyzed bidirectional synthesis of N-heteropolycyclic compounds bearing carbazole moieties – namely π-extended benzodicarbazoles and π-extended indolocarbazoles. Overall, four previously unknown core structures were synthesized. This approach is convergent, modular and the gold-catalyzed key step comprises of a cascade reaction starting from stable di-azido compounds. The obtained molecules were fully characterized and their optical and electronic properties as well as their performance in organic thin-film transistors generated by vacuum deposition were studied. Charge-carrier mobilities of up to 0.3 cm2/Vs were measured. (Figure presented.).
ZnBr2-mediated synthesis of indoles in a ball mill by intramolecular hydroamination of 2-alkynylanilines
Zille, Markus,Stolle, Achim,Wild, Andreas,Schubert, Ulrich S.
, p. 13126 - 13133 (2014)
A method for the intermolecular hydroamination of 2-alkynylanilines in a planetary ball mill is described, which avoids the use of solvents during the reaction. Different additives were tested, whereby ZnBr2 in stoichiometric amounts showed the best performance in terms of yield and selectivity. Furthermore, the materials used for milling balls and beakers as well as the milling time and the rotation frequency were changed in order to achieve the best reaction conditions. As a result, two methods for the synthesis of 2-substituted 1H-indoles are described with their respective advantages and disadvantages. Both methods were used to convert different alkyl and aryl containing 2-ethynylanilines. This journal is the Partner Organisations 2014.
Direct synthesis of polysubstituted quinoline derivatives by InBr 3-promoted dimerization of 2-ethynylaniline derivatives
Sakai, Norio,Annaka, Kimiyoshi,Konakahara, Takeo
, p. 3653 - 3655 (2006)
InBr3 promotes the dimerization of 2-ethynylaniline derivatives containing an unsubstituted terminal carbon leading to the production of polysubstituted quinoline derivatives in good yield.
Optimization of 4,6-Disubstituted Pyrido[3,2-d]pyrimidines as Dual MNK/PIM Inhibitors to Inhibit Leukemia Cell Growth
Han, Yu,Zhang, Huimin,Wang, Shuxiang,Li, Bo,Xing, Kun,Shi, Yuntao,Cao, Hongxue,Zhang, Jian,Tong, Tong,Zang, Jie,Guan, Lihong,Gao, Xiaoxiao,Wang, Yuetong,Liu, Dan,Huang, Min,Jing, Yongkui,Zhao, Linxiang
, p. 13719 - 13735 (2021/10/01)
Mitogen-activated protein kinase-interacting kinases (MNKs) and provirus integration in maloney murine leukemia virus kinases (PIMs) are downstream enzymes of cell proliferation signaling pathways associated with the resistance of tyrosine kinase inhibitors. MNKs and PIMs have complementary effects to regulate cap-dependent translation of oncoproteins. Dual inhibitors of MNKs and PIMs have not been developed. We developed a novel 4,6-disubstituted pyrido[3,2-d]pyrimidine compound 21o with selective inhibition of MNKs and PIMs. The IC50’s of 21o to inhibit MNK1 and MNK2 are 1 and 7 nM and those to inhibit PIM1, PIM2, and PIM3 are 43, 232, and 774 nM, respectively. 21o inhibits the growth of myeloid leukemia K562 and MOLM-13 cells with GI50’s of 2.1 and 1.2 μM, respectively. 21o decreases the levels ofp-eIF4E andp-4EBP1, the downstream products of MNKs and PIMs, as well as cap-dependent proteins c-myc, cyclin D1, and Mcl-1. 21o inhibits the growth of MOLM-13 cell xenografts without causing evident toxicity. 21o represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.
